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Synthesis and Evaluation of New Antagonists of Bacterial Quorum Sensing in Vibrio harveyi |
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| Authors: | Hanjing Peng Yunfeng Cheng Nanting Ni Minyong Li Dr Gaurav Choudhary Han Ting Chou Chung‐Dar Lu Dr Phang?C Tai Dr Binghe Wang Dr |
| Affiliation: | 1. Department of Chemistry and Center for Biotechnology and Drug Design, Georgia State University, P.O. Box 4098, Atlanta, GA 30302‐4098 (USA), Fax: (+1)?404‐413‐5543;2. ;3. Department of Biology, Georgia State University, P.O. Box 4010, Atlanta, GA 30302‐4010 (USA) |
| Abstract: | Bacterial quorum sensing has received much attention in recent years because of its relevance to pathological events such as biofilm formation. Based on the structures of two lead inhibitors (IC50: 35–55 μM ) against autoinducer‐2‐mediated quorum sensing identified through virtual screening, we synthesized 39 analogues and examined their inhibitory activities. Twelve of these new analogues showed equal or better inhibitory activities than the lead inhibitors. The best compound showed an IC50 value of ～6 μM in a whole‐cell assay using Vibrio harveyi as the model organism. The structure–activity relationship is discussed herein. |
| Keywords: | autoinducer‐2 CoMFA drug design inhibitors quorum sensing |